Pharmacological characterization of MCCG and MAP4 at the mGluR1b, mGluR2 and mGluR4a human metabotropic glutamate receptor subtypes

T. Knöpfel*, S. Lukic, T. Leonardt, P. J. Flor, R. Kuhn, F. Gasparini

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

48 Citations (Scopus)

Abstract

The two reported metabotropic glutamate receptor (mGluR) antagonists, α-methyl-cyclopropyl glycine (MCCG) and α-methyl-aminophosphonobutyrate (MAP4) were tested on the mGluR1b, mGluR2 and mGluR4a subtypes of human mGluRs. Neither MCCG (500 μM) nor MAP4 (500 μM) antagonized the activation of mGluR1b by 10 μM quisqualate. MCCG was found to potently antagonize the action of 30 μM (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid [(1S,3R)-ACPD] at mGluR2 (IC50 = 87.5 μM; apparent KD = 25 μM) but did not block the action of 1 μM S-2-amino-4-phosphonobutyric acid at mGluR4a (IC50 > 1 mM). MAP4 was found to be a weak antagonist or partial agonist at mGluR4a (IC50 > 500 μM) and, less potently, also antagonized the action of 30 μM (1S,3R)-ACPD) at mGluR2 (IC50 ~2 mM).

Original languageEnglish
Pages (from-to)1099-1102
Number of pages4
JournalNeuropharmacology
Volume34
Issue number8
DOIs
Publication statusPublished - Aug 1995

User-Defined Keywords

  • (1S,3R)-ACPD
  • antagonism
  • L-AP4
  • Recombinant receptors
  • α-methyl-amino acids

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